This invention relates to the discovery that 3,3-Bis (p-hydroxyphenyl)phthalide is an effective treatment for certain inflammatory skin conditions, especially those of a viral origin, arthritis, rheumatism, and rheumatoid arthritis.
Phenolphthalein has long been known as one of a group of primary diphenylmethane cathartics. The cathartic effect of phenolphthalein was reportedly discovered in 1902 and since that time it has been widely employed in laxative formulas. It is also reported that phenolphthalein is relatively non-toxic. Goodman & Gillman, Pharmacological Basis of Therapeutics (4 Ed. 1977) "Cathartic and Laxatives" pp. 1021 and 1022. Phenolphthalein is also used as an indicator in titrations of mineral and organic acids and most alkalies.
Although inflammatory viral infections may be caused in humans, mammals, and other animals by a wide variety of viruses, a common virus which produces persistently hard to treat conditions is the Herpes Simplex virus. In humans Type I normally produces above-waist infections while Type II produces lesions below the waist, in the genital region. Common manifestations of viral infection, including Herpes Simplex I infections are labialis (cold sores, fever blisters, etc.) pharyngitis, keratitis, skin infections (herpetic whitlow), encephalitis, and chronic ulcerative stomatitis. Herpes Simplex Type II may cause progenitalis oropharyngeal infections, meningitis and encephalitis. Other manifestations of inflammatory viral infections are canker sores, sun blisters and other such skin lesions and ulcerous conditions. In mammals, such as cows, bulls, and sheep, both Types I and II infect eyes, ears, mouth, and upper respiratory systems. Birds, such as parrots, are virally infected in their digestive tracts among other regions, by what is known as New Castle disease.
Inflammatory viral infections have proven very difficult to treat and in many instances are allowed to run their course with symptomatic treatment such as ointments, local anesthetics and the like. Treatment for Herpes Simplex infections includes dusting with bismuth formic iodide, application of camphor spirit, epinephrine, idoxuridine, adenine arabinoside, large doses of steroids and x-ray or grenz ray therapy.
Inflammatory skin conditions (dermatitis) which occur frequently include photodermatitis and actinic dermatitis such as sunburn, actinic keratosis and the like, eczema pruritus, acute and chronic lesions, burning, swelling and blistering. These conditions are also difficult to treat with moisturizing creams, lotions and other topical agents being employed.
Acne is a disease of the pilosebaceous unit which includes the hair follicle and its sebaceous gland. They are most numerous on the face but also are found in abundance on the back, chest and upper arms. (L. Kaminester, "Acne,"Journal of the American Medical Association, May 19, 1978, Volume 239, No. 20, pages 2171-72). Normally the sebaceous glands secrete an oily material called sebum which rises to the top of the hair follicle and then flows out onto the skin surface. Acne occurs when the canals through which the oily sebum flows become plugged up. Bacteria, chiefly Corynebacterium acnes, live in the hair follicles and break down complex fats into triglycerides and free fatty acids.
The plugged hair follicle, or comedo, often ruptures into the lower skin areas and dumps free fatty acids, horn, fat, hair and bacterial products into the dermis, creating a toxic foreign body response which can cause scarring. Recently recommended treatment of acne includes oral antibiotics that effectively decrease the bacterial count of C acnes. These include tetracycline and erythromycin which selectively concentrate around the hair follicles, thus reducing the C acnes count and subsequent inflammation. Those antibiotics may also be applied in topical application. Kaminester reports that topical applications of antibiotics are inferior to orally administered antibiotics and should not be used in severe cases of inflammatory acne. Topical tretinoin and benzoyl peroxide preparations have also had beneficial effects.
Arthritis is the inflammation of a joint usually accompanied by pain. It can result from a number of conditions including infection, trauma, and degenerative joint diseases.
Rheumatism is an acute or chronic condition characterized by soreness and stiffness of muscles, and pain in joints and associated structures.
Rheumatoid arthritis is a systemic disease characterized by inflammatory changes in joints and related structures. It tends to be chronic. There is no specific cure for it and physical therapy and orthopedic measures are often utilized in its treatment. Various special methods of treatment have been tried with diverse degrees of effectiveness.
It is well known that phenolphthalein is highly insoluble in water. When phenolphthalein is ingested into the human body less than 15% of the active drug in solution is absorbed into the blood stream. The rest of the drug is excreted in the feces.
It is an object of this invention to provide a methodology for rendering phenolphthalein readily soluble in either hot or cold water. This solubility not only enhances its ingestibility by and injectability into the human organism or other mammals but also allows for topical applications using aqueous media, or the preparation of capsules or tablets for ingestion by the mammalian organism.
It is an object of the present invention to provide a fast acting, effective treatment of inflammatory viral infections and skin conditions.
It is a further object to provide a topical agent to arrest dermatitis conditions.
It is a further object of this invention to provide a fast, acting, effective treatment of arthritis, rheumatism, and rheumatoid arthritis, and its pain and symptoms.
It is yet a further object of the invention to provide a topical agent which helps prevent and aids in curing acne.